EP 652 009 A1 describes inhibitors of aspartate protease which inhibit the production of beta-amyloid peptides in cell culture and in vivo.
WO 00/69262 discloses a beta-secretase and the use thereof in assays for finding potential active substances for the treatment of AD.
WO 01/00663 discloses memapsin 2 (human beta-secretase) as well as a recombinant catalytically active enzyme. Methods of identifying inhibitors of memapsin 2 are also described.
WO 01/00665 discloses inhibitors of memapsin 2 for the treatment of AD.
WO 03/057721 discloses substituted aminocarboxamides for the treatment of AD.
At present there are no effective treatment methods capable of preventing, stopping or reversing AD.
The objective of the present invention is therefore to provide new substituted 1,2-ethylenediamines which inhibit the cleaving of APP (Amyloid Precursor Protein) mediated by β-secretase.
A further objective of the present invention is to provide physiologically acceptable salts of the compounds according to the invention with inorganic or organic acids.
Another objective of the present invention is to provide pharmaceutical compositions containing at least one compound according to the invention or a physiologically acceptable salt according to the invention, optionally together with one or more inert carriers and/or diluents.
The present invention further relates to pharmaceutical compositions containing one or more, preferably one active substance, which is selected from the compounds according to the invention and/or the corresponding salts, as well as one or more, preferably one additional active substance optionally together with one or more inert carriers and/or diluents.
This invention further relates to the use of at least one of the compounds according to the invention for inhibiting β-secretase.
The invention also sets out to provide new pharmaceutical compositions which are suitable for the treatment or prevention of diseases or conditions associated with the abnormal processing of Amyloid Precursor Protein (APP) or aggregation of Abeta peptide.
The invention also sets out to provide new pharmaceutical compositions which are suitable for the treatment or prevention of diseases or conditions which can be influenced by inhibiting the β-secretase activity.
The invention also sets out to provide new pharmaceutical compositions which are suitable for the treatment and/or prevention of Alzheimer's disease (AD) and other diseases which are associated with the abnormal processing of APP or aggregation of Abeta peptide, as well as diseases which can be treated or prevented by the inhibition of β-secretase, particularly AD.
The invention also relates to a method of inhibiting β-secretase activity.
Further objectives of the present invention will be apparent to the skilled man immediately from the foregoing remarks and those made hereinafter.